Title:
シンバスタチンの改善された製造方法
Document Type and Number:
Japanese Patent JP2004524260
Kind Code:
A
Abstract:
The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following sequential processes comprising: (i) hydrolysis of lovastatin as starting material with potassium t-butoxide in an organic solvent and small amount of water under a mild reaction condition, followed by lactonization of the obtained solid intermediate with preventing from formation of by-products; (ii) protection of an alcohol group with t-butyldimethylsilyl group which can be easily removed with concentrated hydrochloric acid without the formation of by-products; (iii) acylation of the obtained protected intermediate with acyloxytriphenyl phosphonium salt as an acylating agent under a mild reaction condition; and (iv) removal of the silyl protective group with a concentrated hydrochloric acid. The present invention is to provide the improved process of preparing simvastatin expressed by formula 1 environmentally sound, economically efficient, and industrially useful.
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Inventors:
Hong Chun Il
Kim Jun Woo
Shinhaejeong
Kantaewon
Cho Dong Ok
Kim Jun Woo
Shinhaejeong
Kantaewon
Cho Dong Ok
Application Number:
JP2001546231A
Publication Date:
August 12, 2004
Filing Date:
February 27, 2001
Export Citation:
Assignee:
Chun Khun Dan Pharmaceutical Corporation
International Classes:
A44C5/00; A61K31/366; A61P3/06; A61P43/00; C07B53/00; C07D309/30; (IPC1-7): C07D309/30
Attorney, Agent or Firm:
Kosaku Sugimura